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1. 发明授权

US4180672A 2-Organothio-2-cyclopentenones, organothio-cyclopentanes derived therefrom 失效
标题翻译： 2-有机硫代-2-环戊烯酮，衍生自其的有机硫代环戊烷
公开(公告)号：US4180672A
公开(公告)日：1979-12-25
申请号：US775119
申请日：1977-03-07
申请人： Seizi Kurozumi , Takeshi Toru , Makiko Kobayashi , Yoshinobu Hashimoto
发明人： Seizi Kurozumi , Takeshi Toru , Makiko Kobayashi , Yoshinobu Hashimoto
IPC分类号： A61K31/557 , C07C405/00 , C07F7/18 , C07C177/00
CPC分类号： C07F7/1856 , C07C323/52 , C07C405/0033 , C07C2101/08 , C07C2101/10
摘要： Organothiocyclopentanes of the formula ##STR1## wherein E represents >C.dbd.O or ##STR2## in which Z' represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; X represents --S--, --CH.sub.2 --, --CH.dbd.; represents a single or double bond; R' represents a monovalent or divalent organic group containing 1 to 25 carbon atoms; R represents a monovalent organic group containing 1 to 25 carbon atoms; Z represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; and when both E and Z represent a hydroxyl group or a protected hydroxyl group, X represents --S--.Also, 2-organothio-2-cyclopentenones of the formula ##STR3## wherein R and Z are as defined above. The compounds of formula (I) are prepared by reacting 2,3-epoxy-cyclopentanone or its derivatives with mercaptans in the presence of basic compounds. The compounds of formula (II) are prepared by reacting the compounds of formula (I) with mercaptans or organocopper-lithium compounds, and optionally reducing the resulting products, and optionally protecting the hydroxyl group at their cyclopentane ring.The compounds of formula (I) have an action of inhibiting ulcer formation, and are useful intermediates for the compounds of formula (II). The compounds of formula (II) are monothia- or dithia-prostanoic acid derivatives, and exhibit various superior pharmacological actions.
摘要翻译：式（II）的有机硫代环戊烷，其中E表示> C = O或其中Z'表示氢原子，羟基或被保护的羟基的“IMAGE” X表示-S - ， - CH 2 - ， - CH = 代表单键或双键; R'表示含有1〜25个碳原子的一价或二价有机基团; R表示含有1〜25个碳原子的一价有机基团; Z表示氢原子，羟基或保护的羟基; 并且当E和Z都表示羟基或被保护的羟基时，X表示-S-。另外，式（I）的2-有机硫代-2-环戊烯酮其中R和Z如上定义。在碱性化合物的存在下，使2,3-环氧环戊酮或其衍生物与硫醇反应制备式（I）化合物。式（II）化合物通过使式（I）化合物与硫醇或有机锂化合物反应，任选地还原所得产物和任选地保护其环戊烷环上的羟基来制备。式（I）化合物具有抑制溃疡形成的作用，并且是式（II）化合物的有用的中间体。式（II）化合物是单硫酸或二硫氨基 - 前列腺烷酸衍生物，具有各种优异的药理作用。

2. 发明授权

US4008125A New cyclopentene-diols and new acyl esters thereof and process for their preparation 失效
标题翻译：新的环戊烯二醇及其新的酰基酯及其制备方法
公开(公告)号：US4008125A
公开(公告)日：1977-02-15
申请号：US630711
申请日：1975-11-10
申请人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sadakazu Matsubara , Sachio Ishimoto
发明人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sadakazu Matsubara , Sachio Ishimoto
IPC分类号： C07C35/06 , C07C45/67 , C07D309/12 , C07F7/18 , C12N9/18 , C12P7/38 , C12P41/00 , C12D13/02
CPC分类号： C12P41/004 , C07C35/06 , C07C45/67 , C07D309/12 , C07F7/1856 , C12N9/18 , C12P7/38 , Y10S435/917 , Y10S435/942
摘要： New optically active cyclopentene-diol and the mono- or diacyl esters thereof and a process for converting a diacyl ester of cyclopent-1-en-3,5-diol to its monoacyl ester and/or its diol which comprises subjecting a diacyl ester of cyclopent-1-en-3,5-diol containing at least one of the optically active or inactive diacyl ester of trans-cyclopent-1-en-3,5-diol (trans-isomer) and diacyl esters of cis-cyclopent-1-en-3,5-diol (cis-isomer), to the action of a microorganism or enzyme having at least a selectivity in its rates of hydrolyzing the acyloxy group (R) configuration and the acyloxy group (S) configuration of said diacyl ester. These new compounds are valuable as starting materials for the preparation of prostaglandin or its analogues.
摘要翻译：新的光学活性环戊烯二醇及其单 - 或二酰基酯，以及将环戊-1-烯-3,5-二醇的二酰基酯转化成其单酰基酯和/或其二醇的方法，其包括使二含有反式环戊-1-烯-3,5-二醇（反式异构体）的光学活性或无活性二酰基酯和顺式环戊烯-1-烯-3,5-二醇的二酰基酯的环戊-1-烯-3,5-二醇， 1-顺-3,5-二醇（顺式异构体）对于水解所述酰氧基（R）构型和所述酰氧基（R）构型的酰氧基（S）构型）的速率至少具有选择性的微生物或酶的作用二酰基酯。

3. 发明授权

US6020325A Method for inhibiting replication of HIV 失效
标题翻译：抑制HIV复制的方法
公开(公告)号：US6020325A
公开(公告)日：2000-02-01
申请号：US264686
申请日：1999-03-09
申请人： Fujio Suzuki , Hidetaka Sasaki , Makiko Kobayashi
发明人： Fujio Suzuki , Hidetaka Sasaki , Makiko Kobayashi
IPC分类号： A61K31/715 , A61P31/18 , A61K31/70
CPC分类号： A61K31/715
摘要： A method for inhibiting replication of HIV, which comprises subjecting HIV-infected cells to a composition (a) comprising as a primary component a polysaccharide derived from a hot aqueous solvent extract of tubercle bacillus.
摘要翻译：一种用于抑制HIV复制的方法，其包括将HIV感染的细胞对包含作为主要组分的组合物（a）包含衍生自结核杆菌的热水性溶剂提取物的多糖。

4. 发明授权

US6015796A Method for treating AIDS 失效
标题翻译：艾滋病治疗方法
公开(公告)号：US6015796A
公开(公告)日：2000-01-18
申请号：US38041
申请日：1998-03-11
申请人： Fujio Suzuki , Hidetaka Sasaki , Makiko Kobayashi
发明人： Fujio Suzuki , Hidetaka Sasaki , Makiko Kobayashi
IPC分类号： A61K31/715 , A61K45/06 , A61K31/70
CPC分类号： A61K31/715 , A61K45/06
摘要： The present invention relates to a method for treating AIDS, which comprises administering to an HIV-infected patient (a) a composition containing as the primary component a polysaccharide derived from a hot water extract of human-type tubercle bacillus and (b) a nucleoside-type anti-HIV agent. Due to the incorporation of composition (a), the present invention enhances the therapeutic effect of nucleoside-type anti-HIV agents on AIDS.
摘要翻译：本发明涉及一种治疗AIDS的方法，其包括向HIV感染患者施用（a）含有源自人型结核杆菌的热水提取物的多糖作为主要成分的组合物和（b）核苷型抗HIV药物。由于组合物（a）的结合，本发明增强了核苷型抗HIV剂对艾滋病的治疗效果。

5. 发明授权

US4132726A Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives 失效
标题翻译： 4-羟基环戊-2-烯-1-酮衍生物的制备方法
公开(公告)号：US4132726A
公开(公告)日：1979-01-02
申请号：US642800
申请日：1975-12-22
申请人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto , Sadakazu Matsubara
发明人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto , Sadakazu Matsubara
IPC分类号： C07C35/06 , C07C45/67 , C07D309/12 , C07F7/18 , C12P7/38 , C12P41/00
CPC分类号： C07C49/707 , C07C35/06 , C07C45/676 , C07D309/12 , C07F7/1804 , C07F7/1856 , C12P41/004 , C12P7/38 , Y02P20/55
摘要： Novel optically active compounds of 4-protected hydroxy-cyclopent-2-en-1-ones of the formula ##STR1## wherein R is a splittable protective group for an alcoholic hydroxyl group, and a process for preparing the 4-protected hydroxycyclopent-2-en-1-ones by oxidizing monohydroxy-protected derivatives of cyclopent-1-ene-3,5-diol expressed by the following formula ##STR2## wherein R is the same as defined above. Optically active 4-hydroxycyclopent-2-en-1-one which is an optically active isomer of the compound of formula (2); or optically active cyclopent-1-en-3,5-diol (R-isomer) and a novel diacyl derivative of the diol, a novel monoacylmonosilyl-derivative of the diol and a novel monoacylmonotetrahydropyranol-derivative of the diol, which are intermediates for the protective derivative of formula (1). Processes are also provided for preparing the protective derivatives of formula (1) by converting these intermediates by esterification, hydrolysis, enzymatic processes, etc. The optically active compounds of formula (2) are useful as precursors for the preparation of prostaglandin or its analogues.
摘要翻译：新型的具有式（2）的4-保护的羟基 - 环戊-2-烯-1-酮的光学活性化合物，其中R是醇羟基的可裂解的保护基，以及制备4-保护的羟基环戊-2-烯-1-酮通过氧化由下式（1）表示的环戊-1-烯-3,5-二醇的单羟基保护衍生物，其中R与上述定义相同。光学活性的4-羟基环戊-2-烯-1-酮，它是式（2）化合物的旋光异构体; 或光学活性的环戊-1-烯-3,5-二醇（R-异构体）和二醇的新型二酰基衍生物，二醇的新型单酰基单甲硅烷基衍生物和二醇的新型单酰基单四氢吡喃醇衍生物，其为式（1）的保护性衍生物。还提供了通过酯化，水解，酶法等转化这些中间体来制备式（1）的保护性衍生物的方法。式（2）的光学活性化合物可用作制备前列腺素或其类似物的前体。

6. 发明授权

US09548439B2 Porosity control in piezoelectric films 有权
标题翻译：压电薄膜中的孔隙度控制
公开(公告)号：US09548439B2
公开(公告)日：2017-01-17
申请号：US14240168
申请日：2011-08-24
申请人： Makiko Kobayashi , Cheng-Kuei Jen
发明人： Makiko Kobayashi , Cheng-Kuei Jen
IPC分类号： B06B1/06 , H01L41/047 , G01N29/34 , H01L41/187 , H01L41/318 , H01L41/08 , H01L41/331
CPC分类号： B06B1/0662 , B06B1/06 , B06B1/0688 , G01N29/34 , H01L41/0477 , H01L41/0805 , H01L41/183 , H01L41/187 , H01L41/1876 , H01L41/318 , H01L41/331 , H01L41/37 , Y10T29/42
摘要： A piezoelectric film having a porosity between 20 and 40%, a thickness ranging from tens of microns to less than a few millimeters can be used to form an ultrasonic transducer UT for operation in elevated temperature ranges, that emit pulses having a high bandwidth. Such piezoelectric films exhibit greater flexibility allowing for conformation of the UT to a surface, and obviate the need for couplings or backings. Furthermore, a method of fabricating an UT having these advantages as well as better bonding between the piezoelectric film and electrodes involves controlling porosity within the piezoelectric film.
摘要翻译：可以使用具有20至40％之间的孔隙率，几十微米至小于几毫米的厚度的压电膜，以形成在发射具有高带宽的脉冲的高温范围内操作的超声换能器UT。这种压电膜表现出更大的灵活性，允许将UT构造到表面，并且消除对联轴器或背衬的需要。此外，制造具有这些优点的UT以及压电膜和电极之间更好的结合的方法包括控制压电膜内的孔隙率。

7. 发明申请

US20060116337A1 Use of glycyrrhizin and its derivatives as MCP-1 production inhibitors 审中-公开
标题翻译：甘草甜及其衍生物作为MCP-1生产抑制剂的使用
公开(公告)号：US20060116337A1
公开(公告)日：2006-06-01
申请号：US11265328
申请日：2005-11-01
申请人： Fujio Suzuki , Makiko Kobayashi , Tokuichiro Utsunomiya , Hiroatsu Matsumoto , Midori Takeda , Shigemi Iwata
发明人： Fujio Suzuki , Makiko Kobayashi , Tokuichiro Utsunomiya , Hiroatsu Matsumoto , Midori Takeda , Shigemi Iwata
IPC分类号： A61K31/704 , A61K31/235
CPC分类号： A61K31/473 , A61K31/57 , A61K31/704 , A61K31/7052
摘要： The object of the present invention is to provide the use of glycyrrhizin and its derivatives for inhibition of MCP-1 production. The present invention discloses an MCP-1 production inhibition method and pharmaceutical composition for the same comprising administration of glycyrrhizin and its derivatives in an amount effective for said inhibition to mammals in which migration of monocytes or T lymphocytes is increased, or production of IL-10 is increased, and inhibition of said increase is desired, thereby treating or preventing decreases in infection resistance.
摘要翻译：本发明的目的是提供甘草甜素及其衍生物用于抑制MCP-1产生的用途。本发明公开了一种MCP-1产生抑制方法及其药物组合物，其含有对所述抑制单核细胞或T淋巴细胞迁移的哺乳动物有效量的甘草甜素及其衍生物的给药量，或产生IL-10 并且希望抑制所述增加，从而治疗或防止耐感染性降低。

8. 发明授权

US4139717A 1,3-Dicarbonyl compounds 失效
标题翻译： 1,3-二羰基化合物
公开(公告)号：US4139717A
公开(公告)日：1979-02-13
申请号：US756739
申请日：1977-01-04
申请人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto
发明人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto
IPC分类号： C07C45/45 , C07C49/12 , C07C49/76 , C07C405/00 , C07F1/00 , C07F7/18 , C07C65/20 , C07C69/95
CPC分类号： C07F7/1804 , C07C405/00 , C07F1/00
摘要： 1,3-Dicarbonyl compounds useful as medicines, agricultural chemicals, perfumes, and their intermediates are prepared by reacting a specific .alpha.,.beta.-unsaturated carbonyl compound with a specific organic copper lithium compound in the presence of an aprotic inert organic solvent, and then reacting the reaction product with an organic carboxylic acid halide or anhydride. In particular, novel 2-acyl-3-substituted cyclopentan-1-ones and 2-acyl-3-substituted cyclohexan-1-ones having important physiological activities are provided.
摘要翻译：用作药物，农药，香料及其中间体的1,3-二羰基化合物通过在非质子惰性有机溶剂存在下使特定的α，β-不饱和羰基化合物与特定的有机铜锂化合物反应制备，然后使反应产物与有机羧酸卤化物或酸酐反应。特别地，提供了具有重要生理活性的新的2-酰基-3-取代的环戊烷-1-酮和2-酰基-3-取代的环己烷-1-酮。

9. 发明申请

US20110009352A1 RESTORATIVE AGENT FOR ANTIBACTERIAL PEPTIDE PRODUCTION ABILITY 审中-公开
标题翻译：用于抗菌肽生产能力的恢复剂
公开(公告)号：US20110009352A1
公开(公告)日：2011-01-13
申请号：US12831559
申请日：2010-07-07
申请人： Fujio Suzuki , Makiko Kobayashi , Tokuichiro Utsunomiya , Tsuyoshi Yoshida , Shohei Yoshida
发明人： Fujio Suzuki , Makiko Kobayashi , Tokuichiro Utsunomiya , Tsuyoshi Yoshida , Shohei Yoshida
IPC分类号： A61K31/704 , C07H15/256 , A61P43/00
CPC分类号： A61K31/704 , A61K2300/00
摘要： There is provided a medicament capable of enhancing the antimicrobial peptide production ability. The medicament contains, as an active ingredient, a compound which is glycyrrhizin or a pharmaceutically acceptable salt thereof and capable of inhibiting the production of at least one of interleukin-10 (IL-10) and chemokine CCL2. The antimicrobial peptide is preferably defensin or cathelicidin.
摘要翻译：提供能够增强抗微生物肽生产能力的药物。作为活性成分，作为活性成分，含有甘草甜素或其药学上可接受的盐，能够抑制白细胞介素-10（IL-10）和趋化因子CCL2中的至少一种的生成的化合物作为活性成分。抗微生物肽优选为防御素或导管素。

10. 发明授权

US4039563A Process for preparing cyclopent-2-en-1-one derivatives 失效
标题翻译：制备环戊-2-烯-1-酮衍生物的方法
公开(公告)号：US4039563A
公开(公告)日：1977-08-02
申请号：US572287
申请日：1975-04-28
申请人： Toshio Tanaka , Seizi Kurozumi , Takeshi Toru , Shuji Miura , Makiko Kobayashi , Sachio Ishimoto
发明人： Toshio Tanaka , Seizi Kurozumi , Takeshi Toru , Shuji Miura , Makiko Kobayashi , Sachio Ishimoto
IPC分类号： C07C69/738 , C07C51/00 , C07C59/82 , C07C67/00 , C07C69/74 , C07C69/95 , C07C49/46 , C07B3/00
CPC分类号： C07D309/12
摘要： A process for preparing cyclopent-2-en-1-one derivatives of the formula ##STR1## wherein R.sub.1 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group, andR.sub.2 is a hydrogen atom or a substituent which is not substantially brominated under the treating conditions, which comprises treating a cyclopentanone derivative of the formula ##STR2## wherein R.sub.1 and R.sub.2 are the same as defined above, with pyridinium hydrobromide perbromide.
摘要翻译：制备式（I）的环戊-2-烯-1-酮衍生物的方法，其中R1是取代或未取代的烷基或取代或未取代的芳基，R2是氢原子或取代基在处理条件下基本上不溴化，其包括用溴化吡啶鎓过溴化物处理式（II）的环戊酮衍生物，其中R1和R2与上述定义相同。

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